N-(piperidine-1-yl)-4,5-diphenyl-1-methylimidazole-2-carboxamide | 489446-69-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-(piperidine-1-yl)-4,5-diphenyl-1-methylimidazole-2-carboxamide
• 英文别名: N-(piperidin-1-yl)-4,5-diphenyl-1-methylimidazole-2-carboxamide；1-methyl-4,5-diphenyl-N-piperidin-1-ylimidazole-2-carboxamide
• CAS: 489446-69-7
• 化学式: C₂₂H₂₄N₄O
• 分子量: 360.459
• InChiKey: JRZYIQYONIPUER-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4,5-diphenyl-1-methylimidazole-2-carboxylic acid 、 N-(piperidine-1-yl)-4,5-diphenyl-1-methylimidazole-2-carboxamide 在 苯胺 作用下， 生成 1-methyl-4,5-diphenyl-1H-imidazole-2-carboxylic acid anilide
  参考文献：
  名称：

  Substituted imidazoles as cannabinoid receptor modulators

  摘要：

  本发明涉及将这些新型化合物用于选择性拮抗Cannabinoid-1（CB1）受体。因此，本发明的化合物可用作治疗精神病、记忆障碍、认知障碍、偏头痛、神经病、神经炎症性疾病（包括多发性硬化症和吉兰-巴雷综合征）、病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、压力、癫痫、帕金森病和精神分裂症的精神药物。这些化合物还可用于治疗物质滥用障碍，特别是阿片类药物、酒精和尼古丁。这些化合物还可用于治疗与过度食物摄入及相关并发症相关的肥胖或进食障碍。同时还声明了结构式（I）的新型化合物。

  公开号：

  US20030114495A1
• 作为产物：
  描述：

  benzyl 4,5-diphenyl-1-methylimidazole-2-carboxylate 在 palladium on activated charcoal benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 氢气 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 20.0 ℃ 、344.74 kPa 条件下， 生成 N-(piperidine-1-yl)-4,5-diphenyl-1-methylimidazole-2-carboxamide
  参考文献：
  名称：

  Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

  摘要：

  Structure-activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CBI receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 nM) which also demonstrated efficacy in overnight feeding studies in the rat for reduction in both food intake and overall body weight. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.12.078

文献信息

• [EN] 1,4-DIHYDRONAPHTHYRIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE 1,4-DIHYDRONAPHTYRIDINE
  申请人：PFIZER PROD INC

  公开号：WO2009056934A1

  公开（公告）日：2009-05-07

  A compound of formulae (I) or a prodrug of the compound or a pharmaceutically acceptable salt thereof of the compound or prodrug, wherein the substituents are as defined in the specification, pharmaceutical compositions containing the compounds useful as calcium channel antagonists, and to methods of treating heart disease and pain.

  一种化合物的公式（I）或该化合物的前药或其药用可接受的盐或前药，其中取代基如规范中所定义，含有该化合物的药用组合物可用作钙通道拮抗剂，并用于治疗心脏病和疼痛的方法。
• Diaryl Ether Derivatives and Uses Thereof
  申请人：Ruggeri B. Roger

  公开号：US20080070887A1

  公开（公告）日：2008-03-20

  Compounds of Formula (I) that act as antagonists at the mu, kappa and/or delta opioid receptors and therefore useful in the treatment of diseases, conditions and/or disorders that benefit from such antagonism in animals are described herein. where R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are described herein.

  本文描述了具有化学式（I）的化合物，这些化合物在mu、kappa和/或delta阿片受体上起拮抗作用，因此在动物治疗受益于这种拮抗作用的疾病、状况和/或障碍方面具有用处。其中R1、R2、R3、R4、R5和R6如下描述。
• Method of treatment or prevention of obesity
  申请人：Fong M Tung

  公开号：US20050171161A1

  公开（公告）日：2005-08-04

  The present invention relates to a method of treating or preventing obesity (or suppressing the appetite) in a human patient by antagonizing CB1 receptors and inhibiting the enzyme 11β-HSD1 in an amount that is effective to treat or prevent obesity. Compounds useful in the present invention have an ion channel activity level greater than about 2 μM. Preferably the compound is a dual selective inhibitor, selectively antagonizing CB1 receptors and selectively inhibiting the enzyme 11β-HSD1

  本发明涉及一种通过拮抗CB1受体和抑制11β-HSD1酶以有效治疗或预防肥胖（或抑制食欲）的方法。本发明中有用的化合物具有大于约2μM的离子通道活性水平。最好的化合物是双重选择性抑制剂，可以选择性地拮抗CB1受体和选择性地抑制酶11β-HSD1。
• Pyrimido [4,5-D] Azepine Derivatives As 5-HT2C Agonists
  申请人：Andrews Mark

  公开号：US20100113422A1

  公开（公告）日：2010-05-06

  The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof wherein the variables R 1 , R 2 , R 3a , R 3b , R 3b , R 3d , and R 100 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a 5-HT 2c receptor-mediated disorders with a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

  本发明提供了式（I）的化合物：或其药学上可接受的盐，其中变量R1、R2、R3a、R3b、R3b、R3d和R100如本文所定义。本发明还涉及包括式（I）化合物的制药组合物，以及使用式（I）的化合物或包括式（I）的制药组合物治疗5-HT2c受体介导的疾病的方法。
• PPY agonists and uses thereof
  申请人：Pfizer Products Inc.

  公开号：EP2078729A1

  公开（公告）日：2009-07-15

  The invention provides PYY3-36 variants and pegylated derivatives thereof and compositions and methods useful in the treatment of conditions modulated by an NPY Y2 receptor agonist.

  本发明提供了PYY3-36变体及其聚乙二醇化衍生物，以及用于治疗受NPY Y2受体激动剂调节的病症的组合物和方法。